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Approaches to evaluate ADME properties of peptides

20 October 2017

Currently there is an increased interest in peptides in the pharmaceutical research, although peptides represent only a small portion of the current drug market worldwide. Compared to the small molecule drugs, peptides have their pros and cons; they are highly selective, possess high binding affinity toward therapeutic target and minimal drug interaction risk, but they might also suffer from low permeability and the stability problems with short half-life and rapid clearance.

Admescope can support the peptide drug developing companies with ADME services. Metabolic stability can be evaluated by incubating the peptide with whole blood or plasma, S9 fractions (liver, kidney, intestinal) or hepatocytes, followed by UPLC/HR-MS analysis. Also, the stability (half-life) in simulated gastric fluid can be evaluated. Peptide metabolites are generally smaller peptide fragments or amino acids, and they can be identified by UPLC-HR/MS analysis based on their accurate mass. The services for evaluating plasma protein binding are also available, using rapid equilibrium dialysis or ultrafiltration method adjusted for minimal non-specific binding.

The in vivo pharmacokinetics of peptide drugs can be investigated in our in-house animal facilities housing mice and rats. These studies can be performed with various dosing and sampling techniques, and when applying UPLC/HR-MS in bioanalysis, the in vivo metID can be performed later on from the same LC/MS data.